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载姜黄素胍基壳聚糖温敏水凝胶经鼻腔给药的抗抑郁作用。

Anti-depressant effect of curcumin-loaded guanidine-chitosan thermo-sensitive hydrogel by nasal delivery.

机构信息

School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, China.

出版信息

Pharm Dev Technol. 2020 Mar;25(3):316-325. doi: 10.1080/10837450.2019.1686524. Epub 2019 Nov 27.

DOI:10.1080/10837450.2019.1686524
PMID:31661648
Abstract

Curcumin, a polyphenol compound extracted from the roots of plants, possesses anti-depressant effect by regulating the levels of neuroendocrine immunological factors. The purpose of this study was to investigate the anti-depressant effect of curcumin through nasal delivery. The results of phase solubility, Fourier transform infrared spectra, Differential scanning calorimetry, X-ray powder diffractometry and H NMR spectra assays showed that curcumin/hydroxypropyl-β-cyclodextrin complex had been obtained. The viscosity of hydrogel increased rapidly at the temperature range of 29-30 °C through the test of rheological property of Guanidine-Chitosan thermo-sensitive hydrogel. And the hydrogel had good mucoadhesion properties. The cumulative release rate of curcumin was 55% in 10 h in vitro drug release test. Curcumin-loaded (14.6, 29.2, or 58.4 μg/kg) thermo-sensitive hydrogel could reduce the immobility time of mice in force swimming test and tail suspension test, while could not increase the independent behavioral activity of mice. In addition, curcumin-loaded (14.6, 29.2, or 58.4 μg/kg) thermo-sensitive hydrogel could increase the concentration of Norepinephrine, Dopamine, 5-Hydroxytryptamine and their metabolites in hippocampus and striatum. In conclusion, thermo-sensitive hydrogel delivery system can be seen as a promising formulation of curcumin for the treatment of depression through nasal delivery.

摘要

姜黄素是从植物根部提取的多酚化合物,通过调节神经内分泌免疫因子的水平具有抗抑郁作用。本研究旨在通过鼻腔给药来研究姜黄素的抗抑郁作用。相溶解度、傅里叶变换红外光谱、差示扫描量热法、X 射线粉末衍射和 H 核磁共振波谱分析的结果表明,姜黄素/羟丙基-β-环糊精复合物已经形成。通过胍基壳聚糖温敏水凝胶的流变性能测试,发现水凝胶的粘度在 29-30°C 的温度范围内迅速增加。并且水凝胶具有良好的粘膜粘附性能。在体外药物释放试验中,姜黄素的累积释放率在 10 小时内达到 55%。姜黄素负载(14.6、29.2 或 58.4μg/kg)温敏水凝胶可减少小鼠在强迫游泳试验和悬尾试验中的不动时间,而不能增加小鼠的独立行为活动。此外,姜黄素负载(14.6、29.2 或 58.4μg/kg)温敏水凝胶可增加海马和纹状体中去甲肾上腺素、多巴胺、5-羟色胺及其代谢物的浓度。总之,温敏水凝胶给药系统可作为通过鼻腔给药治疗抑郁症的姜黄素有前途的制剂。

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